38175-35-8Relevant academic research and scientific papers
Preparation method of tetrahydropyrrole compound
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, (2020/12/09)
The invention discloses a preparation method of a tetrahydropyrrole compound. According to the preparation method, common easily available 3-methoxybenzaldehyde is used as an initial raw material, a compound 002 is obtained through a Wttig reaction, a cyc
Tetrahydropyrrole compound, preparation method, pharmaceutical composition and application thereof
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, (2019/07/16)
The invention discloses a tetrahydropyrrole compound and a preparation method, a pharmaceutical composition and application thereof. The tetrahydropyrrole compound of the invention is as shown in thegeneral formula (I). The tetrahydropyrrole compound of the invention has an excellent inhibitory effect on the positive symptom of schizophrenia, and has equivalent or stronger efficacy in comparisonwith the positive medicine olanzapine. In addition, the compound of the invention has a dual inhibitory effect on a D2 receptor and a DAT receptor, can effectively treat schizophrenia and improve negative symptoms and cognitive functions, and helps reduce side-effect of centrum and secretion of lactogen.
The Titanium-Mediated Double Reductive Cleavage of Cyclic Sulfonamides for the Synthesis of Aryl Pyrrolidines
Khalifa, Aisha,Evans, Paul
, p. 2969 - 2975 (2019/02/26)
Reduction of a range of benzo-fused cyclic sulfonamides has been accomplished using low-valent titanium. This operationally simple method generates the corresponding aryl-substituted cyclic amines, typically, with good conversion. Notably, unlike our previous Li-NH3-based method, loss of heteroatom-based substituents (X) on the aromatic ring does not readily occur, and the robustness of this method was demonstrated with a synthesis of the Sceletium alkaloid mesembrane.
Synthesis of 3-(3-hydroxyphenyl)pyrrolidine dopamine D3 receptor ligands with extended functionality for probing the secondary binding pocket
Omran, Anahid,Eslamimehr, Shakiba,Crider, A. Michael,Neumann, William L.
, p. 1897 - 1902 (2018/04/10)
A series of 3-(3-hydroxyphenyl)pyrrolidine analogues which incorporate N-alkyl groups and N-butylamide-linked benzamide functionality have been synthesized and their in vitro binding affinities at human dopamine receptors have been evaluated. Our ligand design strategy was to take the 3-(3-hydroxyphenyl)pyrrolidine scaffold and extend functionality from the orthosteric binding site to the secondary binding pocket for enhancing affinity and selectivity for the D3 receptor. The N-alkyl analogues constitute a homologous series from N-pentyl to N-decyl to probe the length/bulk tolerance of the secondary binding pocket of the D3 receptor. Enantiomeric 3-(3-hydroxyphenyl)pyrrolidine analogues were also prepared in order to test the chirality preference of the orthosteric binding site for this scaffold. Benzamide analogues were prepared to enhance affinity and/or selectivity based upon the results of the homologous series.
Oximes and hydrazones that are useful in treating sexual dysfunction
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Page/Page column 40, (2010/02/13)
The present invention relates to oximes and hydrazones of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
